ML241-hydrochloride _p97 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEML241 hydrochlorideCat. No.: HY-19797A分式: CHClNO分量: 408.92作靶点: p97作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 34 mg/mL (83.15 mM)* means soluble, but saturatio

2、n unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4455 mL 12.2273 mL 24.4547 mL5 mM 0.4891 mL 2.4455 mL 4.8909 mL10 mM 0.2445 mL 1.2227 mL 2.4455 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 ML241 hydrochloride种有效的 p97 抑制剂，IC50 值为 100 nM。IC50 & Target IC50: 100 n

3、M (p97) 1体外研究ML241 hydrochloride is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 values of 100 nM. ML241inhibits p97 competitively with respect to ATP with a Ki values of 0.35 M. ML241 (20 M) shows no obviousinhibition of the appr 170 kinases tested. ML241 stabilizes UbG76V-GFP with IC50

4、of 3.5 M 1. ML241 is1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEcytotoxic to HCT15 and SW403 cells, with GI50s of 53 and 33 M after treatment for 24 h, and 13 and 12 Mafter treatment for 72 h, respectively 2.PROTOCOLCell Assay 2 HeLa cells stably expressing ODD-luciferase are seeded onto a 96-w

5、ell white solid bottom plate (5000cells/well) and cells are grown for 16 h. Cells are treated with DMEM containing MG132 (4 M) for 1h andwashed with 100 L PBS twice. DMEM containing 2.5% FBS, cycloheximide (50 g/mL) and ML241 areadded into the well. Four 96-well plates are prepared and one of the pl

6、ates is taken out from incubator ateach time point (70, 90, 120, or 150 min). Luciferin (50 L of 1 mg/mL in PBS) is added into each wellcontaining 50 L of medium and incubated at room temperature with shaking at 500 rpm for 5 min.Luminescence intensity is determined with 0.1 ms integration time on t

7、he Synergy HT Microplate Reader 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chou TF, et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase.ChemMedChem. 2013 Feb;8(2):297-312.2. Chou TF, et al. Selective, reversible inhibitors of the AAA ATPase p97. Probe Reports from the NIH Molecular Libraries Program. April14, 2011.McePdfHeightCaution: Product has not been fully validated for medical applications.For re